当前位置： SCI文献检索 > STEROIDS期刊下所有文献 > Fungal sterol C22-desaturase is not an antimycotic target as shown by selective inhibitors and testing on clinical isolates.

Fungal sterol C22-desaturase is not an antimycotic target as shown by selective inhibitors and testing on clinical isolates.

Abstract：

:Inhibition of concise enzymes in ergosterol biosynthesis is one of the most prominent strategies for antifungal chemotherapy. Nevertheless, the enzymes sterol C5-desaturase and sterol C22-desaturase, which introduce double bonds into the sterol core and side chain, have not been fully investigated yet for their potential as antifungal drug targets. Lathosterol side chain amides bearing N-alkyl groups of proper length are known as potent inhibitors of the enzymes sterol C5-desaturase and sterol Δ(24)-reductase in mammalian cholesterol biosynthesis. Here we present the results of our evaluation of these amides for their ability to inhibit enzymes in fungal ergosterol biosynthesis. In the presence of inhibitor(s) an accumulation of sterols lacking a double bond at C22/23 (mainly ergosta-5,7-dien-3β-ol) was observed in Candida glabrata, Saccharomyces cerevisiae, and Yarrowia lipolytica. Hence, the lathosterol side chain amides were identified as selective inhibitors of the fungal sterol C22-desaturase, which was discussed as a specific target for novel antifungals. One representative inhibitor, (3S,20S)-20-N-butylcarbamoylpregn-7-en-3β-ol was subjected to antifungal susceptibility testing on patient isolates according to modified EUCAST guidelines. But, the test organisms showed no significant reduction of cell growth and/or viability up to an inhibitor concentration of 100μg/mL. This leads to the conclusion that sterol C22-desaturase is not an attractive target for the development of antifungals.

journal_name

Steroids

journal_title

Steroids

authors

Müller C,Binder U,Maurer E,Grimm C,Giera M,Bracher F

doi

10.1016/j.steroids.2015.05.004

subject

Has Abstract

pub_date

2015-09-01 00:00:00

pages

1-6

eissn

0039-128X

issn

1878-5867

pii

S0039-128X(15)00150-6

journal_volume

101

pub_type

杂志文章

相关文献

STEROIDS文献大全
  • Dehydroepiandrosterone fatty acyl esters in high density lipoprotein: interaction with human vascular endothelial cells and vascular responses ex vivo.

    abstract：:Dehydroepiandrosterone (DHEA) fatty acyl esters once incorporated in high density lipoprotein (HDL) induce a stronger vasodilatory response in rat mesenteric arteries ex vivo compared to native HDL. We studied the role of HDL receptor, scavenger receptor class B, type 1 (SR-B1), as well as estrogen and androgen recept...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/j.steroids.2010.12.007

    authors： Paatela H,Vihma V,Jauhiainen M,Mervaala E,Tikkanen MJ

    更新日期：2011-03-01 00:00:00

  • Analysis of derivatised steroids by matrix-assisted laser desorption/ionisation and post-source decay mass spectrometry.

    abstract：:Neutral steroids are difficult to analyse using desorption ionisation methods coupled with mass spectrometry (MS). However, steroids with an unhindered ketone group can readily be derivatised with the Girard P (GP) reagent to give GP hydrazones. Steroid GP hydrazones contain a quaternary nitrogen atom and are readily ...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/j.steroids.2005.08.002

    authors： Khan MA,Wang Y,Heidelberger S,Alvelius G,Liu S,Sjövall J,Griffiths WJ

    更新日期：2006-01-01 00:00:00

  • Molecular analysis of 11 beta-hydroxysteroid dehydrogenase and its role in the syndrome of apparent mineralocorticoid excess.

    abstract：:The syndrome of apparent mineralocorticoid excess (AME) is an inherited form of hypertension in which 11 beta-hydroxysteroid dehydrogenase (11-HSD) is defective. This enzyme converts cortisol to its inactive metabolite, cortisone. The deficiency allows mineralocorticoid receptors to be occupied by cortisol, because th...

    journal_title：Steroids

    pub_type： 杂志文章,评审

    doi：10.1016/s0039-128x(96)00164-x

    authors： White PC,Mune T,Rogerson FM,Kayes KM,Agarwal AK

    更新日期：1997-01-01 00:00:00

  • Synthesis and anticancer activity of novel C6-piperazine substituted purine steroid-nucleosides analogues.

    abstract：:Novel C6-piperazine substituted purine nucleoside analogues (2-9) bearing a modified pyranose-like D ring of the 4-azasteroid moiety were efficiently synthesized through nucleophilic substitution at C6 position of the steroid-nucleoside precursors (1) with versatile piperazines. All newly-synthesized compounds were ev...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/j.steroids.2013.12.004

    authors： Huang LH,Xu HD,Yang ZY,Zheng YF,Liu HM

    更新日期：2014-04-01 00:00:00

  • Cortisol to cortisone: glucocorticoid to mineralocorticoid.

    abstract：:11 beta-hydroxysteroid dehydrogenase (11 beta-HSD), by converting cortisol and corticosterone to hormonally inactive cortisone and 11-dehydrocorticosterone, respectively, is an important pre-receptor signaling pathway for the renal mineralocorticoid receptor (MR). This receptor has an equal affinity for the glucocorti...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/0039-128x(94)00024-7

    authors： Stewart PM,Mason JI

    更新日期：1995-01-01 00:00:00

  • Synthesis, cytotoxic evaluation, and molecular docking studies of the semi-synthetic "triterpenoid-steroid" hybrids.

    abstract：:Synthetic transformations of steroids for drug discovery and improvement of drug effectiveness have been an important part of modern medicinal chemistry and pharmaceutical sciences. Pentacyclic triterpenoids, being represented in the nature by various structures and biogenetically related to steroids, can largely expa...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/j.steroids.2018.10.005

    authors： Tolmacheva IA,Nazarov AV,Eroshenko DV,Grishko VV

    更新日期：2018-12-01 00:00:00

  • Allylic oxidation of steroidal olefins by vanadyl acetylacetonate and tert-butyl hydroperoxide.

    abstract：:Readily available vanadyl acetylacetonate was found to oxidize the allylic sites of Δ(5) steroidal alcohols without protection of hydroxyl groups. Cholesterol, dehydroepiandrosterone, cholesterol benzoate, cholesterol acetate, pregnenolone, and 5-pregnen-3,20-diene were oxidized to 7-keto products using vanadyl acetyl...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/j.steroids.2015.06.005

    authors： Grainger WS,Parish EJ

    更新日期：2015-09-01 00:00:00

  • In human T cells mifepristone antagonizes glucocorticoid non-genomic rapid responses in terms of Na(+)/H(+)-exchange 1 activity, but not ezrin/radixin/moesin phosphorylation.

    abstract：:Glucocorticoids (GCs) and progesterone have been employed as immunosuppressive agents during pregnancy for many years. Intracellular acidification by GCs is due to a rapid non-genomic inhibition of membrane Na(+)/H(+)-exchange 1 (NHE1) activity and is followed by immunosuppression of PHA-stimulated proliferation. NHE1...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/j.steroids.2016.01.004

    authors： Chien EJ,Hsu CH,Chang VH,Lin EP,Kuo TP,Chien CH,Lin HY

    更新日期：2016-07-01 00:00:00

  • Antigen-specific T cell functions are suppressed over the estrogen-dendritic cell-indoleamine 2,3-dioxygenase axis.

    abstract：:Estrogen results in the suppression of experimental allergic encephalomyelitis (EAE), a frequently used experimental animal model of multiple sclerosis (MS). The mechanism by which estrogen acts in diseases with an autoimmune background is less clear. Here, we used splenic dendritic cells (DC) from the Lewis rats EAE ...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/j.steroids.2004.05.019

    authors： Xiao BG,Liu X,Link H

    更新日期：2004-09-01 00:00:00

  • Studies on the mechanism of action of 1 alpha,24-dihydroxyvitamin D3. III. The specific binding of 1 alpha,24-dihydroxyvitamin D3 to the receptor of chick parathyroid gland.

    abstract：:Three protein fractions of the cytosol of the chick parathyroid glands, which had the sedimentation constants of 2.5 S, 3.7 S and 5.5 S, were found to bind with 1 alpha,25-dihydroxyvitamin D3. Among these proteins, the 3.7 S protein was assumed to be the specific receptor protein. The 3.7 S receptor protein was also ...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/0039-128x(82)90125-8

    authors： Ishizuka S,Bannai K,Naruchi T,Hashimoto Y

    更新日期：1982-01-01 00:00:00

  • Membrane estrogen receptors activate metabotropic glutamate receptors to influence nervous system physiology.

    abstract：:Until recently, the idea that estradiol could affect cellular processes independent of nuclear estrogen receptors was often dismissed as artifact. This in spite of a large number of carefully controlled studies performed both within and outside the nervous system demonstrating estrogens regulate various intracellular ...

    journal_title：Steroids

    pub_type： 杂志文章,评审

    doi：10.1016/j.steroids.2008.11.013

    authors： Boulware MI,Mermelstein PG

    更新日期：2009-07-01 00:00:00

  • Nine new steroidal glycosides from the roots of Cynanchum stauntonii.

    abstract：:Nine new steroidal glycosides, named as stauntosides C-K (2, 5, 7-10, 13, 14, and 16), along with seven known compounds (1, 3, 4, 6, 11, 12, and 15) were isolated from the 95% ethanol extract of the roots of Cynanchum stauntonii. The structures of these new compounds were elucidated on the basis of extensive spectrosc...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/j.steroids.2012.10.007

    authors： Yu JQ,Deng AJ,Qin HL

    更新日期：2013-01-01 00:00:00

  • Synthesis and antitumor evaluation of methyl spongoate analogs.

    abstract：:A series of novel methyl spongoate (1) analogs has been synthesized and evaluated for their in vitro cytotoxic properties. It was found that the nature of the C-20 side chain had significant effects on their bioactivities and some analogs showed higher cytotoxicity than 1 against A549, HCT-116, HepG2, SW-1990, MCF-7 a...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/j.steroids.2010.08.002

    authors： Jiang CS,Huang CG,Feng B,Li J,Gong JX,Kurtán T,Guo YW

    更新日期：2010-12-12 00:00:00

  • Invalidation of a commercially available human 5α-dihydrotestosterone immunoassay.

    abstract：:Enzyme immunoassays (EIA) are commonly utilized for the evaluation of androgens in biological fluids; however, careful consideration must be given to cross-reactivity with other endogenous sex-steroid hormones. Our purpose was to determine the validity of a commonly-utilized commercially-available dihydrotestosterone ...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/j.steroids.2013.08.013

    authors： Yarrow JF,Beck DT,Conover CF,Beggs LA,Goldberger BA,Borst SE

    更新日期：2013-12-11 00:00:00

  • Naturally occurring marine steroid 24-methylenecholestane-3β,5α,6β,19-tetraol functions as a novel neuroprotectant.

    abstract：:Steroids have been shown to have multiple effects on the nervous system including neuroprotective activities, and they have the potential to be used for the treatment of neurodegenerative diseases. In this current study, we tested the hypothesis that the marine steroid 24-methylenecholestane-3β,5α,6β,19-tetraol (Tetro...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/j.steroids.2015.11.005

    authors： Leng T,Liu A,Wang Y,Chen X,Zhou S,Li Q,Zhu W,Zhou Y,Su X,Huang Y,Yin W,Qiu P,Hu H,Xiong ZG,Zhang J,Yan G

    更新日期：2016-01-01 00:00:00

  • Simultaneous quantification of progesterone, estrone, estradiol-17 beta and corticosterone in female American kestrel plasma.

    abstract：:Progesterone, estrone, estradiol-17 beta and corticosterone were quantified simultaneously for the first time in female American kestrel (Falco sparverius) plasma. A mean level for each hormone was determined for the laying and non-laying periods of the summer (April-September), and for February. Means were comparable...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/0039-128x(84)90012-6

    authors： Rehder NB,Lague PC,Bird DM

    更新日期：1984-04-01 00:00:00

  • Synthesis of 13C-labeled steroid hormones.

    abstract：:The synthesis of 13C-labeled steroid hormones is reviewed. Two general approaches are highlighted: partial synthesis in which part of the steroid nucleus is replaced with 13C-labeled synthons, and total synthesis. Examples from both approaches, leading to (3-(3)C)-, (4-(13)C)-, (3,4-(13)C2)-, and (1,2,3,4-(13)C4)- lab...

    journal_title：Steroids

    pub_type： 杂志文章,评审

    doi：10.1016/0039-128x(90)90012-z

    authors： Zomer G,Stavenuiter JF

    更新日期：1990-10-01 00:00:00

  • Synthesis of biologically active steroid derivatives by the utility of Lawesson's reagent.

    abstract：:Steroid derivatives V, VI, VII and VIII reacted with Lawesson's reagent (LR) to produce spiro-oxazaphosphole-4',17-androstene derivative XI, diazaphospholoandrostane XIV and the thionated derivatives XVI and XVII, respectively. The structures of the new compounds were confirmed by analytical and spectroscopic evidence...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/j.steroids.2004.11.001

    authors： Mohamed NR,Elmegeed GA,Abd-ElMalek HA,Younis M

    更新日期：2005-03-01 00:00:00

  • Dehydroepiandrosterone sulfate (DHEA-S) and DHEA-S-like compounds in fibrocystic disease of the breast.

    abstract：:We assayed Type 1 (high K+) and Type 2 (high Na+) human breast cyst fluids for DHEA-S. When an antibody specific for the 3-sulfoconjugate end of DHEA-S was used, Type 1 cyst fluids (n = 18) showed a content of 114 +/- 68 micrograms/mL (mean +/- sigma) and Type 2 cyst fluids (n = 14) of 35 +/- 17 micrograms/mL (P less ...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/0039-128x(88)90004-9

    authors： Chasalow FI,Blethen SL,Bradlow HL

    更新日期：1988-09-01 00:00:00

  • Peer group normalization and urine to blood context in steroid metabolomics: the case of CAH and obesity.

    abstract：:Traditional interpretation of GC-MS output involved the semi-quantitative estimation of outstanding low or high specific metabolites and the ratio between metabolites. Here, we utilize a systems biology approach to steroid metabolomics of a complex steroid-related disorder, using an all-inclusive analysis of the stero...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/j.steroids.2014.07.003

    authors： Vitkin E,Ben-Dor A,Shmoish M,Hartmann MF,Yakhini Z,Wudy SA,Hochberg Z

    更新日期：2014-10-01 00:00:00

  • In vivo androgen retention in mouse kidney.

    abstract：:The in vivo retention of 3-H-testosterone, dihydrotestosterone (DHT), 3alpha-androstanediol (3alpha-DIOL), 3beta-DIOL, androstenedione, progesterone and cortisol by renal cytoplasm and nuclei of male and female mice was studied. Testosterone was the major androgen isolated from cytoplasm and nuclei following testoster...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/s0039-128x(75)80011-0

    authors： Bullock LP,Bardin CW

    更新日期：1975-01-01 00:00:00

  • Hydroxycitric acid potentiates the cytotoxic effect of tamoxifen in MCF-7 breast cancer cells through inhibition of ATP citrate lyase.

    abstract：:Hydroxycitric acid (HCA), a dietary-derived weight loss supplement, competitively inhibits ATP citrate lyase (ACLY). Tamoxifen (TAM) is the most frequently used therapy for estrogen receptor (ER)-positive breast cancer patients, but its application was restricted due to efficacy related issues. Lipid metabolic reprogr...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/j.steroids.2020.108656

    authors： Ismail A,Doghish AS,E M Elsadek B,Salama SA,Mariee AD

    更新日期：2020-08-01 00:00:00

  • Peripheral benzodiazepine receptor in cholesterol transport and steroidogenesis.

    abstract：:Steroidogenesis begins with the metabolism of cholesterol to pregnenolone by the inner mitochondrial membrane cytochrome P450 side-chain cleavage (P450scc) enzyme. The rate of steroid formation, however, depends on the rate of cholesterol transport from intracellular stores to the inner mitochondrial membrane and load...

    journal_title：Steroids

    pub_type： 杂志文章,评审

    doi：10.1016/s0039-128x(96)00154-7

    authors： Papadopoulos V,Amri H,Boujrad N,Cascio C,Culty M,Garnier M,Hardwick M,Li H,Vidic B,Brown AS,Reversa JL,Bernassau JM,Drieu K

    更新日期：1997-01-01 00:00:00

  • Sterols of the cultured euglenid Eutreptia viridis: a novel delta 23-unsaturated sterol.

    abstract：:The sterol mixture isolated from the marine alga Eutreptia viridis consists mainly of delta 5,7-dienes which account for 80% of the free sterols. Eighteen different sterols were detected, including a novel sterol with the rare delta 23-unsaturation, viz. 24-ethylcholesta-5,7,23Z-trien-3 beta-o1. ...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/0039-128x(82)90018-6

    authors： Zielinski J,Kokke WC,Fenical W,Djerassi C

    更新日期：1982-10-01 00:00:00

  • Marine sterols. VIII. Isolation and structure of sarcosterol, a new sterol with a delta17(20)-double bond from the soft coral Sarcophyton glaucum.

    abstract：:The sterol mixture of the southern Japan's soft coral, Sarcophyton glaucum, was found to contain 11 sterols including a novel sterol, 23,24 xi-dimethylcholesta-5,22-dien-3 beta-ol and a new diunsaturated C29 sterol. 22,23-Dihydrobrassicasterol and gorgosterol were the major components in free- and esterified sterols r...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/0039-128x(79)90079-5

    authors： Kobayashi M,Tomioka A,Mitsuhashi H

    更新日期：1979-09-01 00:00:00

  • Rat endometrial stromal-epithelial response to estrogen infusion.

    abstract：:Morphologic changes at the interface of rat endometrial luminal epithelial cells and the stromal cells immediately adjacent were examined and correlated with hypertrophy of the epithelial cells during estradiol (E2) infusion (1 microgram E2/24 h). While the lamina densa in castrate endometrium was thread-like, it beca...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/0039-128x(91)90061-y

    authors： Lavia LA,Larson BA

    更新日期：1991-03-01 00:00:00

  • Two new polyhydroxysteroids from the gorgonian Isis hippuris.

    abstract：:Two new polyhydroxysteroids isihippurols A (1) and B (2) were isolated from the MeOH extract of the gorgonian Isis hippuris in addition to nine known steroids namely gorgosterol, 3alpha-acetoxy-24-methyl 11beta,18; 18,20beta; 22,25-triepoxy-5alpha-furostane, hippurin-1, 22-epi-hippuristanol, 22-epi-hippurin-1, 3-acety...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/s0039-128x(01)00098-8

    authors： Shen YC,Prakash CV,Chang YT

    更新日期：2001-09-01 00:00:00

  • Why do humans have two glucocorticoids: A question of intestinal fortitude.

    abstract：:The main purpose of this review article is threefold (a) to try to address the question "why are two adrenal glucocorticoids, cortisol and corticosterone, secreted by humans and other mammalian species?", (b) to outline a hypothesis that under certain physiological conditions, corticosterone has additional biochemical...

    journal_title：Steroids

    pub_type： 杂志文章,评审

    doi：10.1016/j.steroids.2015.06.017

    authors： Morris DJ

    更新日期：2015-10-01 00:00:00

  • A comparison of three methods of hydrolysis for estrogen conjugates.

    abstract：:The efficiencies for estrogen conjugate hydrolysis were compared between enzyme hydrolysis, acid solvolysis and a new method, ammonolysis. Samples included: 1) crystalline 1,3,5(10)-estratriene-3, 17 beta-diol disulfate (estradiol 3,17-disulfate), 2) squirrel monkey urine collected following an intravenous injection o...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/0039-128x(84)90023-0

    authors： Bain JD,Kasman LH,Bercovitz AB,Lasley BL

    更新日期：1984-06-01 00:00:00

  • The use of 6alpha-and 6beta-carboxymethyl testosterone-bovine serum albumin conjugates in radioimmunoassay for testosterone.

    abstract：:The synthesis of 6alpha- and 6beta-testosterone-bovine serum albumin (BSA) conjugates is described. 6beta-Carboxymethyl-4-androstene-3,17-dione was prepared by a route analogous to that described earlier for 6beta-carboxymethyl progesterone. Sodium borohydride reduction of the 3 and 17 keto groups and subsequent selec...

    journal_title：Steroids

    pub_type： 杂志文章

    doi：10.1016/s0039-128x(75)80004-3

    authors： Jones CD,Mason NR

    更新日期：1975-01-01 00:00:00